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大环内酯 XY，一种来源于海洋衍生 18 号菌株的大环内酯抗生素。

Macrolactin XY, a Macrolactin Antibiotic from Marine-Derived sp. 18.

机构信息

Department of Biochemistry and Molecular Biology, College of Basic Medical Sciences, Naval Medical University, Shanghai 200433, China.

出版信息

Mar Drugs. 2024 Jul 23;22(8):331. doi: 10.3390/md22080331.

DOI:10.3390/md22080331
PMID:39195447
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC11355411/
Abstract

Two new compounds, macrolactin XY () and (5, 9, 10)-5-(hydroxymethyl)-1,3,7-decatriene-9,10-diol (), together with nine known compounds (-) were isolated from the marine sp. 18 by the OSMAC strategy. These compounds were evaluated for antibacterial activity against six tested microorganisms. Compounds - and - showed varied antibacterial activity, with the minimum inhibitory concentration (MIC) ranging from 3 to 12 μg/mL. Macrolactin XY () was found to possess superior antibacterial activity, especially exhibiting significant effectiveness against . The antibacterial activity mechanism against was investigated. The mechanism may disrupt bacterial cell membrane integrity and permeability, and also inhibit the expression of genes associated with bacterial energy metabolism, as established by the experiments concerning cell membrane potential, SDS-PAGE electrophoresis, cell membrane integrity, and key gene expressions. This study offers valuable insights and serves as a theoretical foundation for the future development of macrolactins as antibacterial precursors.

摘要

两种新化合物，大环内酯 XY（）和（5,9,10）-5-（羟甲基）-1,3,7-癸三烯-9,10-二醇（），与其他 9 种已知化合物（-）一起从海洋真菌 18 中通过 OSMAC 策略分离得到。这些化合物被评估了对六种测试微生物的抗菌活性。化合物 - 和 - 表现出不同的抗菌活性，最小抑菌浓度（MIC）范围为 3 至 12 μg/mL。大环内酯 XY（）被发现具有优越的抗菌活性，特别是对 表现出显著的效果。研究了其对 的抗菌活性机制。该机制可能通过破坏细菌细胞膜的完整性和通透性，并抑制与细菌能量代谢相关的基因表达，通过细胞膜电位、SDS-PAGE 电泳、细胞膜完整性和关键基因表达的实验来确定。这项研究为大环内酯作为抗菌前体的未来发展提供了有价值的见解和理论基础。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/c106/11355411/6ce3a125abe8/marinedrugs-22-00331-g007.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/c106/11355411/8704cd98c7c0/marinedrugs-22-00331-g001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/c106/11355411/6d7eaad5bb92/marinedrugs-22-00331-g002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/c106/11355411/20e701b5b21f/marinedrugs-22-00331-g003.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/c106/11355411/0810bbcb9928/marinedrugs-22-00331-g004.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/c106/11355411/afafdf46a032/marinedrugs-22-00331-g005.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/c106/11355411/cebe6fffd79e/marinedrugs-22-00331-g006.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/c106/11355411/6ce3a125abe8/marinedrugs-22-00331-g007.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/c106/11355411/8704cd98c7c0/marinedrugs-22-00331-g001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/c106/11355411/6d7eaad5bb92/marinedrugs-22-00331-g002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/c106/11355411/20e701b5b21f/marinedrugs-22-00331-g003.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/c106/11355411/0810bbcb9928/marinedrugs-22-00331-g004.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/c106/11355411/afafdf46a032/marinedrugs-22-00331-g005.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/c106/11355411/cebe6fffd79e/marinedrugs-22-00331-g006.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/c106/11355411/6ce3a125abe8/marinedrugs-22-00331-g007.jpg

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